Tazemetostat
Sarcoma
.svg)
Drug Status
Government Approvals
US(FDA)
WHO Essential Medicine
NO
Known Teratogen
NO
Pharmaceutical Class
Methyltransferase Inhibitor
Controlled Drug Substance
No
Tazemetostat
Summary
Tazemetostat is used to treat epithelioid sarcoma and certain types of follicular lymphoma in patients 16 years and older.
Tazemetostat works by inhibiting an enzyme called EZH2. This enzyme plays a role in the growth and spread of cancer cells. By blocking this enzyme, Tazemetostat helps to stop the proliferation of cancer cells, potentially slowing disease progression.
The recommended dosage of Tazemetostat for both adults and children aged 16 years and older is 800 mg taken orally twice daily.
Common side effects of Tazemetostat include fatigue, nausea, decreased appetite, and vomiting. Serious adverse effects can include secondary malignancies such as myelodysplastic syndrome and acute myeloid leukemia.
Key warnings for Tazemetostat include the risk of secondary malignancies and embryofetal toxicity. Patients should be monitored for new cancers and pregnant women should avoid this medication due to potential harm to the fetus.
Indications and Purpose
How does Tazemetostat work?
Tazemetostat works by inhibiting the EZH2 enzyme, which is involved in the methylation of histone proteins, leading to the repression of gene expression. By blocking this enzyme, Tazemetostat disrupts the growth and spread of cancer cells, particularly in conditions where EZH2 is overactive or mutated, such as in certain types of lymphoma and sarcoma.
Is Tazemetostat effective?
Tazemetostat has shown efficacy in treating epithelioid sarcoma and follicular lymphoma. In clinical trials, it demonstrated an overall response rate of 15% in epithelioid sarcoma patients and 69% in patients with EZH2 mutant follicular lymphoma. These results indicate its potential effectiveness, although continued approval may depend on further verification of clinical benefits.
What is Tazemetostat?
Tazemetostat is used to treat epithelioid sarcoma and certain types of follicular lymphoma in patients 16 years and older. It works by inhibiting the EZH2 enzyme, which plays a role in the growth and spread of cancer cells. By blocking this enzyme, Tazemetostat helps to stop the proliferation of cancer cells, potentially slowing disease progression.
Directions for Use
For how long do I take Tazemetostat?
Tazemetostat is typically taken until disease progression or unacceptable toxicity occurs. The duration of use can vary significantly depending on the individual's response to treatment and the specific condition being treated. Regular monitoring by a healthcare provider is essential to determine the appropriate length of treatment.
How do I take Tazemetostat?
Tazemetostat should be taken orally twice a day, with or without food. It is important to swallow the tablets whole without cutting, crushing, or chewing them. Patients should avoid consuming large amounts of grapefruit or grapefruit juice while taking this medication, as it can affect how the drug works.
How long does it take for Tazemetostat to start working?
The time it takes for Tazemetostat to start working can vary depending on the individual and the condition being treated. In clinical trials, the median time to response for patients with EZH2 mutant follicular lymphoma was 3.7 months, while for those with wild-type follicular lymphoma, it was 3.9 months. Regular monitoring by a healthcare provider is essential to assess the medication's effectiveness.
How should I store Tazemetostat?
Tazemetostat should be stored in its original container, tightly closed, and kept out of reach of children. It should be stored at room temperature, away from excess heat and moisture, and not in the bathroom. Proper storage ensures the medication remains effective and safe to use.
What is the usual dose of Tazemetostat?
The recommended dosage of Tazemetostat for both adults and children aged 16 years and older is 800 mg taken orally twice daily. This dosage is consistent for treating both epithelioid sarcoma and follicular lymphoma. It is important to follow the prescribed dosage and consult a healthcare provider for any adjustments.
Warnings and Precautions
Can I take Tazemetostat with other prescription drugs?
Tazemetostat interacts with strong or moderate CYP3A inhibitors, which can increase its plasma concentrations and potentially lead to more severe side effects. It is advised to avoid coadministration with these inhibitors. Additionally, Tazemetostat can decrease the efficacy of CYP3A substrates, including hormonal contraceptives, so alternative birth control methods should be used.
Can Tazemetostat be taken safely while breastfeeding?
Women are advised not to breastfeed during treatment with Tazemetostat and for one week after the final dose. This recommendation is due to the potential risk of serious adverse reactions in the breastfed child, although there is no specific data on the presence of Tazemetostat in human milk.
Can Tazemetostat be taken safely while pregnant?
Tazemetostat can cause fetal harm based on animal studies and its mechanism of action. Pregnant women should avoid using this medication, and females of reproductive potential should use effective non-hormonal contraception during treatment and for 6 months after the final dose. There is no strong evidence from human studies, but the potential risk to the fetus is significant.
Is Tazemetostat safe for the elderly?
Clinical studies of Tazemetostat did not include sufficient numbers of patients aged 65 and over to determine whether they respond differently from younger subjects. Therefore, elderly patients should use Tazemetostat with caution, and healthcare providers should closely monitor them for any adverse effects or changes in efficacy.
Who should avoid taking Tazemetostat?
Key warnings for Tazemetostat include the risk of secondary malignancies and embryo-fetal toxicity. Patients should be monitored for new cancers, and pregnant women should avoid this medication due to potential harm to the fetus. Additionally, Tazemetostat may interact with other drugs, so it's important to inform healthcare providers of all medications being taken.
